1jty
From Proteopedia
(New page: 200px<br /><applet load="1jty" size="450" color="white" frame="true" align="right" spinBox="true" caption="1jty, resolution 2.97Å" /> '''Crystal structure of...) |
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| - | [[Image:1jty.gif|left|200px]]<br /><applet load="1jty" size=" | + | [[Image:1jty.gif|left|200px]]<br /><applet load="1jty" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="1jty, resolution 2.97Å" /> | caption="1jty, resolution 2.97Å" /> | ||
'''Crystal structure of the multidrug binding transcriptional regulator QacR bound to ethidium'''<br /> | '''Crystal structure of the multidrug binding transcriptional regulator QacR bound to ethidium'''<br /> | ||
==Overview== | ==Overview== | ||
| - | The Staphylococcus aureus multidrug binding protein QacR represses | + | The Staphylococcus aureus multidrug binding protein QacR represses transcription of the qacA multidrug transporter gene and is induced by structurally diverse cationic lipophilic drugs. Here, we report the crystal structures of six QacR-drug complexes. Compared to the DNA bound structure, drug binding elicits a coil-to-helix transition that causes induction and creates an expansive multidrug-binding pocket, containing four glutamates and multiple aromatic and polar residues. These structures indicate the presence of separate but linked drug-binding sites within a single protein. This multisite drug-binding mechanism is consonant with studies on multidrug resistance transporters. |
==About this Structure== | ==About this Structure== | ||
| - | 1JTY is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Staphylococcus_aureus Staphylococcus aureus] with ET and SO4 as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http:// | + | 1JTY is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Staphylococcus_aureus Staphylococcus aureus] with <scene name='pdbligand=ET:'>ET</scene> and <scene name='pdbligand=SO4:'>SO4</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1JTY OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Staphylococcus aureus]] | [[Category: Staphylococcus aureus]] | ||
| - | [[Category: Brennan, R | + | [[Category: Brennan, R G.]] |
| - | [[Category: Brown, M | + | [[Category: Brown, M H.]] |
[[Category: Grkovic, S.]] | [[Category: Grkovic, S.]] | ||
| - | [[Category: Miller, M | + | [[Category: Miller, M C.]] |
| - | [[Category: Schumacher, M | + | [[Category: Schumacher, M A.]] |
| - | [[Category: Skurray, R | + | [[Category: Skurray, R A.]] |
[[Category: ET]] | [[Category: ET]] | ||
[[Category: SO4]] | [[Category: SO4]] | ||
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[[Category: transcription]] | [[Category: transcription]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 13:26:43 2008'' |
Revision as of 11:26, 21 February 2008
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Crystal structure of the multidrug binding transcriptional regulator QacR bound to ethidium
Overview
The Staphylococcus aureus multidrug binding protein QacR represses transcription of the qacA multidrug transporter gene and is induced by structurally diverse cationic lipophilic drugs. Here, we report the crystal structures of six QacR-drug complexes. Compared to the DNA bound structure, drug binding elicits a coil-to-helix transition that causes induction and creates an expansive multidrug-binding pocket, containing four glutamates and multiple aromatic and polar residues. These structures indicate the presence of separate but linked drug-binding sites within a single protein. This multisite drug-binding mechanism is consonant with studies on multidrug resistance transporters.
About this Structure
1JTY is a Single protein structure of sequence from Staphylococcus aureus with and as ligands. Full crystallographic information is available from OCA.
Reference
Structural mechanisms of QacR induction and multidrug recognition., Schumacher MA, Miller MC, Grkovic S, Brown MH, Skurray RA, Brennan RG, Science. 2001 Dec 7;294(5549):2158-63. PMID:11739955
Page seeded by OCA on Thu Feb 21 13:26:43 2008
